hdl cholesterol

Dalcetrapib (RO4607381) 是rhCETP 抑制剂(IC50:0.2 μM)，具有增加血浆中HDL 胆固醇含量的作用。

Gemfibrozil (CI-719) 是一种PPAR-α激活剂，可作为降脂药。它也是P450非选择性抑制剂，对 CYP2C9、2C19、2C8 和 1A2 的Ki 值分别为 5.8、24、69 和 82 μM。

CETP-IN-3 is an inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP.

Gemcabene calcium , a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) andexerting anti-inflammatory activity, lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP).

Anacetrapib (MK-0859) 是 CETP 的抑制剂，能够抑制 rhCETP (IC50:7.9±2.5 nM) 和 C13S CETP 突变型 (IC50:11.8±1.9 nM) 的活性。

是胆固醇酯转移蛋白 (CETP) 选择性抑制剂。根据人血浆的抑制曲线，Torcetrapib (CP-529414) 对CETP 的最有效浓度为 37 nM。

Brl 26314 can elevate HDL-cholesterol in rats.

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

Methyl protodioscin (Smilax saponin B) 是一种甾二糖苷，能诱导细胞周期阻滞，具有抗肿瘤活性。

Evacetrapib (LY2484595) 是 CETP 的选择性抑制剂，在人血浆中，抑制人重组 CETP 蛋白 (IC50:5.5 nM) 和 CETP (IC50:36 nM) 活性。

Obicetrapib potassium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.

Obicetrapib calcium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.

Obicetrapib sodium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.

Bambuterol is a prodrug of β2-agonist commonly used for the treatment of asthma and chronic obstructive pulmonary disease (COPD) with the advantage of once daily dosing and favorable side effect profile. Administration of a single-dose of R-bambuterol resulted in dose-dependent reductions in the levels of plasma LDL-C, high-density lipoprotein cholesterol (HDL-C), total cholesterol (TC), apolipoprotein B (ApoB) and apolipoprotein A1 (ApoA1) at Tmax. R-bambuterol can lower the plasma levels of LDL-C, and marginally raise the ratio of ApoA1 ApoB (indicator of HDL-C LDL-C) with both a single dose and multiple doses. R-bambuterol was more potent in LDL-C lowering than rac-bambutero

GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.

Azalanstat HCl is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat HCl has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg kg day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Azalanstat mesylate is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat mesylate has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg kg day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

SP4e是一种PPAR-γ激活剂，在HK-2细胞中EC50=826.7 nM。在瑞士白化病小鼠模型中，SP4e能有效降低血糖、总胆固醇、甘油三酯和低密度脂蛋白水平，增加高密度脂蛋白水平。

RG33是一种33个氨基酸的合成肽，与apolipoprotein A1 (ApoA1)的C-末端域中两个Y类螺旋的209-219和220-241氨基酸相对应。它能溶解含有1,2-dimyristoyl-sn-glycero-3-PC (DMPC)的多层囊泡(MLVs)，形成重组HDL。与脂质结合的RG33在J774巨噬细胞中诱导胆固醇外流。RG33 (12 mg/kg)可降低胰岛素抵抗性小鼠的血糖水平。

CS-6253TFA为CS-6253的TFA盐类,具有作用于ATP结合盒1 (ABCA1) 的激动剂功能.该化合物能有效调节淀粉样蛋白β的Aβ42 40比率,对血浆中的脂蛋白代谢产生影响.此外,CS-6253 TFA能够促进富含胆固醇的高密度脂蛋白(HDL)颗粒的产生,并触发微粒的释放.

CS-6253是一种ATP结合盒1 (ABCA1) 的激动剂,具有改善淀粉样蛋白βAβ42 40比率的功能,并对血浆中的脂蛋白代谢产生影响.此外,CS-6253还能生成富含胆固醇的高密度脂蛋白 (HDL) 颗粒,并诱导微粒释放.

Alpinumisoflavone has atheroprotective effects, may result from their ability to upregulate mechanisms promoting HDL-cholesterol and bile acid formation, it is endowed with estrogenic properties accounting, at least in part, for E. lysistemon effects. Alp